Electron-Deficient Fluoroarene-Mediated Synthesis of Trifluoromethyl Ketones from Carboxylic Acids.

Fluoroarene-mediated trifluoromethylation of carboxylic acids for the synthesis of trifluoromethyl ketones is disclosed. The fluoroarene activates the acid group and generates the fluoride source in situ for the trifluoromethylation reaction. The present protocol is safe and metal-free, operates under mild reaction conditions, and does not require any external additives to generate trifluoromethyl anion. The current transformation provides good functional group tolerance and also delivers 92% and 88% yields of trifluoromethyl ketones in batch and continuous flow, respectively.

Effect of tert-alcohol functional imidazolium salts on oligomerization and fibrillization of amyloid ß (1-42) peptide.

Imidazolium based IL's has gained vast interest in developing biological applications. Oligomerization and fibrillization of amyloid ß (1-42) peptide are mainly responsible for the extra-neuronal deposition of amyloid fibrils in neurodegenerative disorders like Alzheimer's disease (AD). Here, we report an effect of tert-BuOH-functional imidazolium ILs on oligomerization and fibrillization of amyloid ß (1-42) Peptide in vitro. In this study, a series of these [alkyl-tOHim][OMs] ILs with methyl sulphonate counter anion by varying alkyl chains were used. Among the seven protic ILs, four showed strong binding and inhibition activity for the formation of amyloid ß (1-42) aggregation by using Thioflavin T fluorescence binding assay. The secondary structural analysis of the peptide, pre-incubated with active ILs shows the loss of ordered ß-sheet amyloid structure. The longer alkyl chain ILs showed that an increased in amyloid binding and hence an inhibition effect on amyloid aggregation was enhanced. Thus, we propose that ILs could be presented as potential candidates for therapeutic intervention against Alzheimer's disease (AD).